Synthesis and Anti-Breast Cancer Evaluation of Novel N-(Guanidinyl)benzenesulfonamides

被引：21

作者：

Wu, Jin ^{[1
]}

Zhong, Daixing ^{[2
]}

Fu, Xijin ^{[1
]}

Liu, Qingjun ^{[1
]}

Kang, Liangqi ^{[1
]}

Ding, Zhenqi ^{[1
]}

机构：

[1] Xiamen Univ, Affiliated Southeast Hosp, Dept Orthopaed, Zhangzhou 363000, Peoples R China

[2] Fourth Mil Med Univ, Affiliated Tangdu Hosp, Dept Thorac Surg, Xian 710038, Peoples R China

来源：

INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES | 2014年 / 15卷 / 04期

关键词：

sulfonamides; heterocycles; structure-activity relationships; antitumor agents; GO POTASSIUM CHANNEL; PROGNOSTIC-FACTORS; OSTEOSARCOMA; ETHER; EAG1; EXPRESSION; SARCOMA; OVEREXPRESSION; PROLIFERATION; ANGIOGENESIS;

D O I：

10.3390/ijms15045570

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

A series of 4-(substituted)-N-(guanidinyl)benzenesulfonamides bearing biologically active pyrazole, pyrimidine and pyridine moieties were prepared and evaluated for their anticancer activity against human tumor breast cell line (MCF7). These sulfonamides showed promising activity with IC50 values ranging from 49.5 to 70.2 mu M. The structure-activity relationship of the synthesized compounds was studied. Interestingly, it was found that the most potent compounds in this study were the corresponding 2-cyanoacrylate 3, 3-oxobutanoate 4, pyrazole 6, pyridine 9 and pyrazole 13. Compounds 7 and 8 are nearly as active as Doxorubicin as reference drug with (IC50 values = 70.2, 68.1 mu M), while compounds 5, 10 and 11 exhibited a moderate activity.

引用

页码：5570 / 5581

页数：12

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